A 61603 hydrobromide
Potent α-adrenoceptor agonist that is at least 35-fold more potent at α1A than at α1B or α1D sites. Induces dose response increases in spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nmol/L). Also available as part of the α1-Adrenoceptor Tocriset™.
|Storage||Desiccate at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solubility||Soluble to 50 mM in water|
Preparing Stock Solutions
The following data is based on the product molecular weight 390.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.56 mL||12.81 mL||25.62 mL|
|5 mM||0.51 mL||2.56 mL||5.12 mL|
|10 mM||0.26 mL||1.28 mL||2.56 mL|
|50 mM||0.05 mL||0.26 mL||0.51 mL|
References are publications that support the biological activity of the product.
Knepper et al (1995) A-61603, a potent α1-adrenergic receptor agonist, selective for the α1A receptor subtype. J.Pharmacol.Exp.Ther. 274 97 PMID: 7616455
Luo et al (2007) Receptor subtype involved in α1A-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta.Pharmacol.Sin. 28 968 PMID: 17588332
Meyer et al (1996) Synthesis and in vitro characterisation of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective α1A receptor agonist. J.Med.Chem. 39 4116 PMID: 8831777
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12 Citations for A 61603 hydrobromide
Citations are publications that use Tocris products. Selected citations for A 61603 hydrobromide include:
Copik et al (2015) Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. PLoS One 10 e0115701 PMID: 25606852
Jensen et al (2010) Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. Naunyn Schmiedebergs Arch Pharmacol 382 475 PMID: 20857090
Amirak et al (2013) p90 ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to G(q)-protein-coupled receptor stimuli, endothelin-1 and α(1)-adrenergic receptor agonists. Biochem J 450 351 PMID: 23215897
Montgomery (2017) An Alpha-1A Adrenergic Receptor Agonist Prevents Acute Doxorubicin Cardiomyopathy in Male Mice. Plos One 12 e0168409 PMID: 28081170
Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -estradiol in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951
Thomas et al (2016) The α-1A Adrenergic Receptor in the Rabbit Heart. Nephrol Dial Transplant 11 e0155238 PMID: 27258143
Thomas et al (2016) A Myocardial Slice Culture Model Reveals Alpha-1A-Adrenergic Receptor Signaling in the Human Heart. JACC Basic Transl Sci 1 155 PMID: 27453955
Desir and Peixoto (2014) Renalase in hypertension and kidney disease. Circ Res 29 42604 PMID: 24137013
Jensen et al (2009) The α-1D Is the predominant α-1-adrenergic receptor subtype in human epicardial coronary arteries. PLoS One 54 1137 PMID: 19761933
Dash et al (2011) A molecular MRI probe to detect treatment of cardiac apoptosis in vivo. Magn Reson Med 66 1152 PMID: 21360750
O-Uchi et al (2008) Interaction of α1-adrenoceptor subtypes with different G proteins induces opposite effects on cardiac L-type Ca2+ channel. PLoS One 102 1378 PMID: 18467629
Rokosh and Simpson (2002) Knockout of the alpha 1A/C-adrenergic receptor subtype: the alpha 1A/C is expressed in resistance arteries and is required to maintain arterial blood pressure. Proc Natl Acad Sci U S A 99 9474 PMID: 12093905
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.